Protease activated receptors: theme and variations

Oncogene. 2001 Mar 26;20(13):1570-81. doi: 10.1038/sj.onc.1204194.


The four PAR family members are G protein coupled receptors that are normally activated by proteolytic exposure of an occult tethered ligand. Three of the family members are thrombin receptors. The fourth (PAR2) is not activated by thrombin, but can be activated by other proteases, including trypsin, tryptase and Factor Xa. This review focuses on recent information about the manner in which signaling through these receptors is initiated and terminated, including evidence for inter- as well as intramolecular modes of activation, and continuing efforts to identify additional, biologically-relevant proteases that can activate PAR family members.

Publication types

  • Research Support, U.S. Gov't, P.H.S.
  • Review

MeSH terms

  • Amino Acid Sequence
  • Binding Sites
  • Endopeptidases / metabolism*
  • GTP-Binding Proteins / metabolism*
  • Models, Biological
  • Molecular Sequence Data
  • Receptor, PAR-2
  • Receptors, Thrombin / metabolism*
  • Signal Transduction*


  • Receptor, PAR-2
  • Receptors, Thrombin
  • Endopeptidases
  • GTP-Binding Proteins